NEW ZEALAND DATA SHEET

POLARAMINE

(dexchlorpheniramine maleate)

DESCRIPTION
Polaramine (dexchlorpheniramine maleate) is the dextro-isomer of chlorpheniramine
maleate. It is an antihistamine with anticholinergic properties

Dexchlorpheniramine maleate (CAS no. 2438-32-6) is described chemically as (+)-2-[p-

chloro--[2-(dimethylamino)ethyl]benzyl]pyridine maleate (1:1).

It has the empirical formula of C16H19ClN2.C4H4O4 and the following structural formula:

Dexchlorpheniramine maleate is a white, odourless, crystalline powder which in aqueous

solution has a pH of between 4 and 5. It is freely soluble in water, soluble in alcohol and in
chloroform, but only slightly soluble in benzene or ether.

PHARMACOLOGY

Pharmacodynamics

Mechanism of Action:
Dexchlorpheniramine, the d-isomer of the racemic compound chlorpheniramine, is two times
more active than chlorpheniramine. Dexchlorpheniramine does not prevent the release of
histamine, but rather, competes with free histamine for binding at the H1-receptor sites, and
competitively antagonizes the effects of histamine on H1-receptors in the GI tract, uterus,
large blood vessels, and bronchial muscle. Blockade of H1-receptors also suppresses the
formation of oedema, flare, and pruritus that result from histaminic activity. Since
dexchlorpheniramine binds to central and peripheral H1-receptors, sedative effects are likely
to occur. H1-antagonists are structurally similar to anticholinergic agents and therefore
possess the potential to exhibit anticholinergic properties of varying degrees. They also
have antipruritic effects. Dexchlorpheniramine has high antihistaminic activity, moderate
anticholinergic effects and minimal sedative effects. The drug does not possess antiemetic
properties.

Pharmacokinetics:
The absorption, distribution, metabolism and elimination of dexchlorpheniramine have not
been specifically described. However, since dexchlorpheniramine is the primary active
isomer of the racemic compound chlorpheniramine, the pharmacokinetics of
dexchlorpheniramine are likely to be similar to that of chlorpheniramine.
 Polaramine Data Sheet
dated 1 October 2014

Dexchlorpheniramine is administered orally. H1-antagonists are generally well absorbed

from the GI tract. The onset of action of immediate release formulations of chlorpheniramine
is about 30-60 minutes. The Cmax of chlorpheniramine occurs in about 2 hours, the
maximum therapeutic effect in about 6 hours, and the duration of action lasts between 4-8
hours. Protein binding is approximately 72%. Chlorpheniramine is widely distributed in body
tissues and fluids, and it crosses the placenta and is excreted into breast milk.

The metabolism of chlorpheniramine is extensive and rapid, first occurring in the gastric
mucosa and then on first-pass through the liver, which may be saturable. N-dealkylation
produces several metabolites, which are excreted in the urine along with the parent
compound. The half-life in healthy adults and children is 20-24 hours and 10-13 hours,
respectively. Excretion rates are dependent on the pH of urine and urinary flow, with the
rate decreasing as the pH rises and urinary flow decreases.

INDICATIONS
POLARAMINE is indicated for symptomatic treatment of perennial and seasonal allergic
rhinitis, vasomotor rhinitis, allergic conjunctivitis, mild uncomplicated allergic skin
manifestations of urticaria and angioedema. Polaramine may relieve itching due to skin
conditions such as allergic eczema, pruritus ani, pruritus vulvae, atopic dermatitis, contact
dermatitis, insect bites, dermographism and drug reactions, including serum sickness.

CONTRAINDICATIONS
Polaramine is contraindicated for use in:
newborns and premature infants.
patients taking monoamine oxidase inhibitors (MAOIs) (see Interactions with other
medicines section)
patients with a history of hypersensitivity to dexchlorpheniramine, to other drugs of
similar chemical structure, or to any other excipients.

PRECAUTIONS
Polaramine may cause drowsiness and may add to the effects of alcohol. Drowsiness may
continue the following day. Those affected should not drive or operate machinery; alcohol
should be avoided.

Polaramine should be used with caution in patients with:

narrow-angle glaucoma
stenosing peptic ulcer
prostatic hypertrophy
bladder neck obstruction
pyloroduodenal obstruction
cardiovascular disease including hypertension
increased intraocular pressure
hyperthyroidism
use with caution in patients with renal or hepatic impairment
seizures

Polaramine may cause photosensitivity in some patients.

Use in Pregnancy (Category A)

Safety during pregnancy has not been established. Polaramine should be used during the
first two trimesters of pregnancy only if clearly needed.
Dexchlorpheniramine maleate should not be used in the third trimester of pregnancy
because newborn and premature infants may have severe reactions to antihistamines.

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 Polaramine Data Sheet
dated 1 October 2014

Polaramine has been taken by a large number of pregnant women and women of
childbearing age without any proven increase in the frequency of malformations or other
direct or indirect harmful effects of on the foetus having been observed.

Use in Lactation
Polaramine is excreted in breast milk. Therefore caution should be exercised when
administered to nursing mothers.

Paediatric use
Children may experience paradoxical excitation with dexchlorpheniramine maleate. In
children this may cause excitability.
Polaramine Syrup contains Sorbitol which may have a laxative effect or cause diarrhoea.

Use in the elderly

The elderly may experience paradoxical excitation with dexchlorpheniramine maleate. In
patients over 60 years of age, antihistamines may cause dizziness, sedation and
hypotension. Also they are more likely to have central nervous system (CNS) depressive
side effects, including confusion.

Interactions with other medicines

The following interactions with Polaramine have been noted:
central nervous system (CNS) depressants (alcohol, sedatives, opioid analgesics,
hypnotics) may cause an increase in sedative effects of Polaramine
concomitant administration with tricyclic antidepressants (TCAs) may result in additive
antimuscarinic activity
monoamine oxidase inhibitors (MAOIs) may prolong and intensify the anticholinergic and
CNS depressive effects of some antihistamines and may cause a decrease in blood
pressure
oral anticoagulants may have their actions decreased by antihistamines.

Effect on laboratory tests

Antihistamines should be discontinued approximately 48 hours prior to skin testing
procedures since these drugs may prevent or diminish otherwise positive reactions to dermal
reactivity indicators.

ADVERSE REACTIONS
Slight to moderate drowsiness is the most frequent side effect of dexchlorpheniramine
maleate.

Other reported reactions associated with antihistamine therapy in general include:

General: Urticaria, drug rash, anaphylactic shock, photosensitivity, excessive

perspiration, chills, dryness of mouth, nose and throat
Cardiovascular: Hypotension, hypertension, headache, palpitations, tachycardia,
extrasystoles
Haematological: Haemolytic anaemia, hypoplastic anaemia, thrombocytopenia,
agranulocytosis
Gastrointestinal: Epigastric distress, anorexia, nausea, vomiting, diarrhoea,
constipation
Genitourinary: Urinary frequency, difficult urination, urinary hesitation and retention,
early menses
Nervous System: Sedation, dizziness, disturbed coordination, fatigue, confusion,
restlessness, excitation, nervousness, tremor, irritability, insomnia,
euphoria, paraesthesia, blurred vision, diplopia, vertigo, tinnitus, acute

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 Polaramine Data Sheet
dated 1 October 2014

labyrinthitis, hysteria, neuritis, convulsions, lassitude, depression,

inability to concentrate, dilated pupils, hypereflexia, hyporeflexia,
xerostomia, hallucinations, appetite stimulation, anxiety, facial
dyskinesias and seizures
Respiratory: Thickening of bronchial secretions, tightness of chest, wheezing, nasal
stuffiness

DOSAGE AND ADMINISTRATION

Polaramine Colour Free Tablets
Adults and children over 12 years: One tablet every 6 hours

Polaramine Syrup
Adults and children over 12 years: 5 mL every 6 hours
Children 6 12 years: 2 4 mL every 6 - 8 hours
Children 4 - 6 years: 1.75 2 mL every 6 - 8 hours
Children 2 4 years: 1.25 1.75 mL every 6 - 8 hours

Polaramine Syrup is not to be used in children under 2 years of age.

OVERDOSAGE
In case of overdose, immediately contact the Poisons Information Centre (in Australia, call
13 11 26; in New Zealand, call 0800 764 766) for advice.

Manifestations. Antihistamine overdosage effects may vary from central nervous system
depression (apnoea, arrhythmias, cardiovascular collapse, cyanosis, diminished mental
alertness, sedation) to stimulation (convulsions, hallucinations, insomnia or tremors) to
death. Other signs and symptoms may be ataxia, blurred vision, dizziness, hypotension and
tinnitus. Stimulation is particularly likely in children, as are atropine-like signs and symptoms
(dry mouth; fixed, dilated pupils; flushing; gastrointestinal symptoms and hyperthermia).

Treatment: Dialysis is of little value in antihistamine poisoning. Treatment of the signs and
symptoms of an over dosage are symptomatic and supportive. Consider standard measures
to remove any unabsorbed drug. There is no specific antidote. Measures to enhance
excretion (urinary acidification, haemodialysis) are not recommended.

PRESENTATION AND STORAGE CONDITIONS

Polaramine is available for oral use as either as: film coated immediate release tablet
(Polaramine Colour Free Tablets) or as a syrup (Polaramine syrup).

Polaramine Colour Free Tablets

Off-white, round, bevelled tablet with Flask and Bowl logo on one side, score on the other
side.
Available in blister packs of 20 and 40 tablets
Active: Dexchlorpheniramine maleate 2 mg
Inactive: Lactose, starch-maize, starch pregelatinised maize, magnesium stearate
Store below 25C

Polaramine Syrup
A clear, red syrup with an orange like odour
Available in a bottle of 100 mL
Active: Dexchlorpheniramine maleate 2mg per 5 mL
Inactive: Sodium citrate, sodium chloride, sucrose, sorbitol solution (70 per cent),
methyl hydroxybenzoate, propyl hydroxybenzoate, menthol, ethanol, water, brilliant
scarlet 4R, apricot flavour, blood orange flavour.
Store below 25C

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 Polaramine Data Sheet
dated 1 October 2014

MEDICINE CLASSIFICATION
Pharmacist Only Medicine

NAME AND ADDRESS

Bayer New Zealand Limited
P. O. Box 2825
Shortland Street
Auckland 1140

Ph: (09) 443 3093 or 0800 847 874

Fax: (09) 443 3094

DATE OF PREPARATION
1 October 2014

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